TAARGain. Innovative medicines
for brain treatment.

A project by the team of Raul Gainetdinov, an internationally recognized pioneer in amine receptor research. The project is aimed at the development of drugs that use the effects of trace TAAR amines on brain receptors.

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Mission

The discovery in 2001 of a new class of monoaminergic receptors associated with trace amines opened a new chapter in the development of innovative drugs that radically change human life. Through the efforts of our team of professionals, we carry out a search for pharmaceutical agents for the treatment of a wide range of socially significant human pathologies

Achievements

Key events in the history of research and development in the field of TAAR.

2014

Compound Validation

At St. Petersburg State University, a research program is being successfully implemented under the project “Validation of TAAR2, TAAR5 and TAAR6 trace amine receptors as potential new drug targets for the treatment of brain diseases” within the framework of the Russian Science Foundation grant No. 14-25-00065.

2015

TAAR knockout animals

In the laboratory of Gainetdinov R.R. in St. Petersburg State University has been created a unique collection of TAAR knockout animals in the world. There are TAAR1, TAAR2, TAAR5 and TAAR6 knockout mice, TAAR9 knockout rats, and TAAR8 knockout mice are being developed. Methods for searching for new TAAR ligands in vitro have been developed.

The presence of the above collection of knockouts makes it possible to greatly reduce the cost of preclinical development of the studied substances, since expensive pharmacodynamic studies will be carried out on the basis of the ITBM of St. Petersburg State University.

2016

BRET in In vitro screening

A platform has been developed for in vitro screening (using the BRET method) of TAAR agonists.

2017

TAAR1 agonists

Original compounds were screened and a number of TAAR1 agonists with nanomolar activity were found.

2018

Pharmaceutical development

Work is underway on the pharmaceutical development of a finished dosage form of the TAAR1 agonist. A plan for preclinical and clinical studies has been developed.

2019

Presidential Grant

In 2019, the laboratory of Gainetdinov R.R. was won the 2019 competition for the event “Conducting research by world-class scientific laboratories as part of the implementation of the priorities of scientific and technological development of the Russian Federation” of the Presidential program of research projects implemented by leading scientists, including young scientists, under a grant from the Russian Science Foundation. Grant topic: “Development of innovative drugs based on TAAR trace amine receptors.”

2021

Expanding horizons

In parallel, the laboratory is conducting fundamental research on other TAARs, the function of which has currently been little studied, but the possible potential for pharmacology is great.

The pharmaceutical giants could do without us, but they need leads in the form of preliminary data from basic research on receptors; except us, scientists, no one will get this data.

Raul Gainetdinov

Scientific director of the TAARGain project

Trace amines

Trace amines are endogenous amines that are present in vertebrate tissues or fluids at concentrations up to 100 ng/g tissue and selectively bind to one or more TAARs at these concentrations. The first trace amines described, B-phenylethylamine, tyramine, tryptamine, and p-octopamine (classical trace amines), show molecular similarities to the known monoamine neurotransmitters dopamine, epinephrine, norepinephrine, and serotonin. In addition to classical trace amines, their derivatives are described, as well as diamines and polyamines, which are found in the body of mammals, but their functions are not completely clear. Trace amines also enter the human body with food and are synthesized by the symbiotic intestinal microbiota. It is important to note that the content of trace amines in human tissues and model animals changes in some pathologies (schizophrenia, ADHD, ulcerative colitis, epilepsy, etc.), which undoubtedly deserves close attention from the point of view of new targets for psychopharmacology in these diseases.

TAARGain. Innovative medicinesfor brain treatment.

TAARGain. Innovative medicines
for brain treatment.